One-Pot Approach to 1,2-Disubstituted Indoles via Cu(II)-Catalyzed Coupling/Cyclization under Aerobic Conditions and Its Application for the Synthesis of Polycyclic Indoles

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• 作者：Jilong Gao ; Yingying Shao ; Jiaoyan Zhu ; Jiaqi Zhu ; Hui Mao ; Xiaoxia Wang ; Xin Lv
• 刊名：Journal of Organic Chemistry
• 出版年：2014
• 出版时间：October 3, 2014
• 年：2014
• 卷：79
• 期：19
• 页码：9000-9008
• 全文大小：604K
• ISSN：1520-6904

文摘

A straightforward assembly of 1,2-disubstituted indoles has been developed through a Cu(II)-catalyzed domino coupling/cyclization process. Under aerobic conditions, a wide range of 1,2-disubstituted indole derivatives were efficiently and facilely synthesized from 2-alkynylanilines and boronic acids. 2-(2-Bromoaryl)-1-aryl-1H-indoles, which were selectively generated in one pot under the Cu catalysis, afforded the indolo[1,2-f]phenanthridines via Pd-catalyzed intramolecular direct C(sp²)鈥揌 arylation. The one-pot tandem approaches to the polycyclic indole derivatives were also successfully achieved.